Patents Issued in March 27, 2018
  • Method for catalytic dehydration of glycerol to acrolein
    Patent number: 9926253
    Abstract: A novel method for catalytic dehydration of glycerol to acrolein is provided. A fixed bed reactor is used, which is placed in a microwave unit. The feedstock is introduced into the fixed bed reactor after being preheated and gasified. Continuous glycerol dehydration occurs in the presence of a microwave-absorbing catalyst in the fixed bed reactor to form acrolein. The microwave-absorbing catalyst is composed of an active component loaded on a core-shell structure which consists of microwave absorbent coated by an oxide. The uniformity of microwave heating can reduce the formation of hot spot during the reaction and hence improve the catalyst stability. The process and operation is simple, and the unit can steadily run for a long time.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: March 27, 2018
    Assignee: ZHEJIANG UNIVERSITY OF TECHNOLOGY
    Inventors: Yong Nie, Qinglong Xie, Ruchao Gong, Ying Duan, Shanshan Li, Yang Liu, Xiaojiang Liang, Zhenyu Wu, Meizhen Lu, Fengwen Yu, Jianbing Ji
  • Process and system for making cyclohexanone
    Patent number: 9926254
    Abstract: Disclosed are processes and systems for making cyclohexanone from a mixture comprising phenol, cyclohexanone, and cyclohexylbenzene comprising a step of or a device for subjecting at least a portion of the mixture to hydrogenation and a step of or a device for distilling a phenol/cyclohexanone/cyclohexylbenzene mixture to obtain an effluent rich in cyclohexanone.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: March 27, 2018
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: Christopher L. Becker, Jason D. Davis, Jihad M. Dakka, Kirk C. Nadler
  • High-purity dibasic acid compositions and methods of making the same
    Patent number: 9926255
    Abstract: High-purity dibasic acid compositions are generally disclosed. In some embodiments, the dibasic acid compositions are solutions or suspensions. In some other embodiments, the compositions are solid-state compositions. In some such embodiments, the solid-state compositions include a dibasic acid as a crystalline solid and further include a low quantity of certain impurities, such as monobasic acids, various esters, and the like. Methods and systems for making such high-purity dibasic acid compositions are also disclosed.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: March 27, 2018
    Assignee: Elevance Renewable Sciences, Inc.
    Inventors: Alpeshkumar K. Patel, Brian Pease, Bradon J. Dreyer, Yenamandra Viswanath, Brian Albert, Steven A. Cohen
  • Catalytic conversion of lactic acid to acrylic acid
    Patent number: 9926256
    Abstract: Disclosed herein is a mixed phosphate catalyst for converting lactic acid to acrylic acid, which is characterized by a high conversion of lactic acid, a high selectivity for acrylic acid, a high yield of acrylic acid, and correspondingly low selectivity and molar yields for undesired by-products. This is achieved with a particular class of catalysts defined by a mixture of metal-containing phosphate salts. Further, the catalyst is believed to be stable and active for lengthy periods heretofore unseen in the art for such dehydration processes.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: March 27, 2018
    Assignee: The Procter & Gamble Company
    Inventors: Janette Villalobos Lingoes, Dimitris Ioannis Collias
  • Continuous process for the preparation of (S)-2-acetyloxypropionic acid chloride
    Patent number: 9926257
    Abstract: The present invention relates to a continuous method for the preparation of (S)-2-acetyloxypropionic acid from an aqueous solution of lactic acid and acetic anhydride, in acetic acid. (S)-2-acetyloxypropionic acid is used for the preparation of (S)-2-acetyloxypropionic acid chloride, an essential intermediate compound for the preparation of lopamidol and has to be industrially produced with high purity and suitable quality for producing lopamidol according to the Pharmacopoeia requirements. The continuous process according to the invention, comprises therefore also the chlorination steps of (S)-2-acetyloxypropionic acid with thionyl chloride to give the corresponding (S)-2-acetyloxypropionic acid chloride which is further distilled to give the suitable purity characteristics for its use for the preparation of non-ionic iodinated contrast agents as lopamidol.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: March 27, 2018
    Assignee: BRACCO IMAGING S.P.A.
    Inventors: Silvia Ceragioli, Pietro Delogu, Armando Mortillaro, Alfonso Nardelli, Stefano Sguassero, Rosario Velardi, Carlo Felice Viscardi
  • Photolabile pro-fragrances
    Patent number: 9926258
    Abstract: The invention relates to specific ketones of formula (I) which act as photolabile pro-fragrances. The invention further relates to detergents or cleaning agents, cosmetic agents and air freshening products including ketones of said type. The invention also relates to a method for lastingly scenting surfaces and a method for lastingly fragrancing rooms using said ketones.
    Type: Grant
    Filed: August 9, 2016
    Date of Patent: March 27, 2018
    Assignee: Henkel AG & Co. KGaA
    Inventors: Christian Kropf, Thomas Gerke, Ursula Huchel, Axel Griesbeck, Agnieszka Landes
  • Catalyst for fixed bed aniline rectification residue recycling and preparation method
    Patent number: 9926259
    Abstract: The present invention relates to a catalyst for fixed bed aniline rectification residue recycling and preparation method thereof. Based on the total weight of the catalyst, the catalyst comprises the following components in percentage by weight: 5-40% of an active component, 2-30% of a first cocatalyst component, 10-30% of a second cocatalyst component and the balance of carrier, wherein the active component is NiO; the first cocatalyst component is one or more of Fe, Mo, Cr or Co oxide; and the second cocatalyst component is one or more of La, Zr, Y or Ce oxide. The catalyst is prepared through co-precipitation. The catalyst shows high activity and stability in the waste liquid treatment process, and can still maintain high rectification residue cracking rate after reaction of 200 hours.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: March 27, 2018
    Assignee: Wanhua Chemical Group Co., Ltd.
    Inventors: Hua Mei, Hao Chen, Dewei Yu, Congying Zhang, Hui Wang, Yuan Li, Zhongying Chen, Zilin Ni, Qingmei Jiang, Shanjian Cao, Zaigang Yang, Jun Qu, Jinhong Song, Bingbo Hu
  • Polyamine transport selective therapeutic agents with enhanced stability
    Patent number: 9926260
    Abstract: Disclosed herein are di-substituted aryl polyamine compounds and methods of making and using the same. The di-substituted polyamine compounds act as PTS targeting agents, which selectively target the polyamine transport system (PTS) with high efficacy and have improved stability in the presence of amine oxidases.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: March 27, 2018
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: Otto Phanstiel, IV, Aaron Muth
  • Bacterial efflux pump inhibitors
    Patent number: 9926261
    Abstract: Disclosed herein are compounds of formula I: and salts thereof. Also disclosed are compositions comprising of compounds of formula I and methods using compounds of formula I.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: March 27, 2018
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Ajit K. Parhi, Gifty A. Blankson, Malvika Kaul, Daniel S. Pilch
  • EP4 agonists as therapeutic compounds
    Patent number: 9926262
    Abstract: Described herein are compounds that are EP4 agonists and antagonists which are useful for treating a variety of pathological conditions associated with activity of EP4 receptors.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: March 27, 2018
    Assignee: ALLERGAN, INC.
    Inventors: David W. Old, Christopher D. Hein
  • Solvent medium for diazotization reaction
    Patent number: 9926263
    Abstract: A solvent medium for diazotization reaction includes a mixed solution of polyethylene glycol and water. The molecular weight of polyethylene glycol is 200-600, and the volume ratio of polyethylene glycol and water is 1:0.4-1.5. The mixed solution also includes hydrochloric acid or sulfuric acid, and the concentration of H+ in the mixed solution is 0.32-1.72 mol L?1.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: March 27, 2018
    Assignee: NANTONG TEXTILE & SILK INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
    Inventors: Jiajie Long, Xiaochen Wei, Ming Shen
  • Phenylcarbamate derivatives as formyl peptide receptor modulators
    Patent number: 9926264
    Abstract: The present invention relates to N-phenyl carbamate derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide 2 receptor.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: March 27, 2018
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, Michael E. Garst
  • Cyclic process for producing taurine
    Patent number: 9926265
    Abstract: There is disclosed a process for producing taurine from ammonium isethionate by the ammonolysis of alkali isethionate in the presence of alkali ditaurinate or alkali tritaurinate, or their mixture, to inhibit the formation of byproducts and to continuously convert the byproducts of the ammonolysis reaction to alkali taurinate. Alkali taurinate is reacted with ammonium isethionate to obtain taurine and to regenerate alkali isethionate. The production yield is increased to from 90% to nearly quantitative. The ammonolysis reaction is catalyzed by alkali salts of hydroxide, sulfate, sulfite, phosphate, or carbonate.
    Type: Grant
    Filed: April 24, 2017
    Date of Patent: March 27, 2018
    Assignee: VITAWORKS IP, LLC
    Inventor: Songzhou Hu
  • Pure isophthalaldehyde bisulfite adduct and novel preparation method thereof
    Patent number: 9926266
    Abstract: Disclosed are a method for preparing a pure isophthalaldehyde bisulfite adduct free from impurities through a specific purification process, and use thereof as a starting material for polymerizing polybenzimidazole under a mild condition. According to the present disclosure, it is possible to obtain a pure isophthalaldehyde bisulfite adduct free from impurities, such as unreacted materials or byproducts. In addition, it is possible to accomplish industrial mass production of a high-molecular weight polybenzimidazole by using the adduct as a starting material for polymerizing polybenzimidazole under a mild condition in an organic solvent.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: March 27, 2018
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyoung-Juhn Kim, Eun Ki Kim, So Young Lee, Jong Hyun Jang, Jin Young Kim, Sung Jong Yoo, Dirk Henkensmeier, Dae Ki Choi, Jonghee Han, Suk Woo Nam
  • Covalent inhibitors of K-Ras G12C
    Patent number: 9926267
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: March 27, 2018
    Assignee: Araxes Pharma LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Method for preparing azetidinone compound and intermediate of azetidinone compound
    Patent number: 9926268
    Abstract: Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: March 27, 2018
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Yuncai Zhang, Xufei Li, Yong Zhang, Dezhou Xu, Li Zhang, Xiaojie Xu, Qifeng Zhu, Xiaoming Wang, Zhiqing Yang, Zehua Zhong, Jian Zhang
  • Beta-lactam cholesterol absorption inhibitors
    Patent number: 9926269
    Abstract: The present invention relates to the novel compounds represented by Formula (Ia) or (Ib) and to their pharmaceutical preparations for the treatment of atherosclerosis and cholesterol level reduction.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: March 27, 2018
    Assignee: RUDJER BOSKOVIC INSTITUTE
    Inventors: Ivan Habus, Tonko Drazic
  • Process for production of glycopyrronium tosylate
    Patent number: 9926270
    Abstract: Provided herein are methods for the production of glycopyrronium tosylate and glycopyrronium tosylate compositions. Also provided herein are compositions useful in the production of glycopyrronium tosylate. Additionally provided herein are glycopyrronium tosylate compositions. Glycopyrronium tosylate is useful for the treatment of, among other conditions, hyperhidrosis.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: March 27, 2018
    Assignee: DERMIRA, INC.
    Inventors: Anthony Adrian Shaw, Enrico Vigano, Renato Molteni
  • Octahydrocyclopentapyrroles, their preparation and use
    Patent number: 9926271
    Abstract: The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: March 27, 2018
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Nicoleta Dobri, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 9926272
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: March 27, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Composition and methods for modulating a kinase cascade
    Patent number: 9926273
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relates to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: March 27, 2018
    Assignee: Athenex, Inc.
    Inventor: David G. Hangauer, Jr.
  • Process for producing substituted methylamine compound and triazine derivative
    Patent number: 9926274
    Abstract: The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group, R represents a hydrogen atom, or an organic group, L represents a halogen atom and the like, and n represents an integer of 2 to 20).
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: March 27, 2018
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yasushi Shibata, Tsutomu Imagawa
  • Allosteric modulators of the cannabinoid 1 receptor
    Patent number: 9926275
    Abstract: The present technology relates to compounds and compositions of Formulas I, II, VII, and VIII, and methods using such compounds. The compounds and compositions described herein may be used in the treatment or prophylaxis of addiction, metabolic syndrome, obesity, and/or a CB1 receptor-mediated disorder.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: March 27, 2018
    Assignee: Northeastern University
    Inventors: Ganeshsingh Arjunsingh Thakur, Ritesh B. Tichkule, Pushkar Mukund Kulkarni, Abhijit Raghunath Kulkarni
  • Substituted benzamides with activity towards EP4 receptors
    Patent number: 9926276
    Abstract: The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: March 27, 2018
    Assignee: DRACONIS PHARMA, S.L.
    Inventors: Marina Virgili Bernado, Elena Carceller Gonzalez, Jordi Salas Solana
  • Pyridone compounds, pharmaceutical compositions thereof, and their therapeutic use for treating proliferative diseases
    Patent number: 9926277
    Abstract: Provided herein are pyridone compounds, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: March 27, 2018
    Assignee: BioTheryX, Inc.
    Inventors: Robert Sullivan, Sara Howard, Leah Fung, Kyle W. H. Chan, Frank Mercurio
  • Sulfonyl hydrazide compounds and a regio-selective process to prepare 4-aroyl pyrazole derivatives
    Patent number: 9926278
    Abstract: Disclosed are compounds of Formula I, including all stereoisomers, (N-oxides), and salts thereof, wherein A and R are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula I, comprising reacting a compound of Formula II with an aroyl enolate salt of Formula III in the presence of an acid in an aqueous solvent mixture, wherein A, R and M are as defined in the disclosure.
    Type: Grant
    Filed: April 14, 2015
    Date of Patent: March 27, 2018
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Kanu Maganbhai Patel
  • Process for the preparation of 3-haloalkylpyrazoles
    Patent number: 9926279
    Abstract: The present invention provides a process for the preparation of a compound of formula I: wherein R1 is C1-C4 haloalkyl; R2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and R3 is methyl or ethyl; comprising reacting a compound of formula IV: wherein R1, R2 and R3 are as defined for the compound of formula I; with an alkylating agent in the presence of an amide.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: March 27, 2018
    Assignee: Syngenta Participations AG
    Inventors: Linhua Wang, Ritesh Bharat Sheth
  • Hydantoins that modulate BACE-mediated APP processing
    Patent number: 9926280
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: March 27, 2018
    Assignee: Buck Institute for Research on Aging
    Inventors: Varghese John, Dale E. Bredesen
  • 5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
    Patent number: 9926281
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: March 27, 2018
    Assignees: GALAPAGOS NV, LES LABORATOIRES SERVIER
    Inventors: Franck Laurent Brebion, Luke Jonathan Alvey, David Amantini, Frédéric André De Ceuninck, Pierre Marc Marie Joseph Deprez, Romain Luc Marie Gosmini, Hélène Marie Jary, Christophe Peixoto, Iuliana Ecaterina Pop-Botez, Marie Laurence Claire Varin
  • Phthalazinones and isoquinolinones as rock inhibitors
    Patent number: 9926282
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 27, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan, Vladimir Ladziata
  • Intermediate compound for preparing rosuvastatin calcium and method for preparing rosuvastatin calcium therefrom
    Patent number: 9926283
    Abstract: Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: March 27, 2018
    Assignees: Asymchem Laboratories (Tianjin) Co., Ltd., Asymchem Life Science (Tianjin) Co., Ltd., Tianjin Asymchem Pharmaceutical Co., Ltd., Asymchem Laboratories (Fuxin) Co., Ltd., Jilin Asymchem Laboratories Co., Ltd.
    Inventors: Hao Hong, James Gage, Jiuyuan Li, Litao Shen, Lei Zhang, Changming Dong
  • Substituted N-(1,2,4-triazol-3-yl)Arylcarboxamide compounds and their use as herbicides
    Patent number: 9926284
    Abstract: The invention relates to N-(1,2,4-triazol-3-yl)arylcarboxamides of formula I and their use as herbicides. In said formula I, X represents N or CR2, whereas R1, R2, R3, R4, R5, R6 and R7 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: March 27, 2018
    Assignee: BASF SE
    Inventors: Frederick Calo, Markus Kordes, Helmut Kraus, Thomas Mietzner, Thomas Seitz, Klaus Kreuz, Maciej Pasternak, Trevor William Newton, Dario Massa
  • Allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 9926285
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Andrew John Harvey, Ian M. Bell
  • Vortioxetine intermediate and synthesis process thereof
    Patent number: 9926286
    Abstract: The present invention provides a new intermediate II and a method for synthesizing the same. The method comprises: (a) firstly diazotizing a compound of formula I as a raw material, and then halogenating to obtain an intermediate II; and (b) reacting the intermediate II with a compound III to obtain a compound IV, hydrolyzing the obtained compound IV directly without being separated to obtain Vortioxetine represented by compound V. The intermediate II can be used for synthesizing Vortioxetine.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: March 27, 2018
    Assignees: SHANGHAI SYNCORES TECHNOLOGIES INC. LTD., ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
    Inventors: Caide Tang, Gang Wang, Boyu Wang, Luning Huang, Eric Gu
  • Purification of taxanes
    Patent number: 9926287
    Abstract: A method of crystallizing docetaxel is disclosed. The method comprises (a) combining docetaxel and at least one solubilizing solvent to obtain a solution, wherein the solubilizing solvent is selected from the group consisting of acetone, methyl-tert-butyl ether, tetrahydrofuran (THF), and acetonitrile and (b) adding an anti-solvent to the solution to obtain a crystalline docetaxel, wherein the anti-solvent is water.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: March 27, 2018
    Assignee: Phyton Holdings, LLC
    Inventors: Brian A. Bucher, Edward M. Desimone, III, Roland R. Franke, Rex T. Gallagher, Barry J. Hand, Christopher D. Howe, James H. Johnson, John S. Juchum, Marc A. Plante, T.G. Sambandam, Dong S. Yang
  • Five-membered cyclic biscarbonates bearing amide linkages, their preparation and their uses for the preparation of polymers
    Patent number: 9926288
    Abstract: A compound is of formula (I): in which A1 and A1? are independently from each other a linear or branched alkylene radical including from 1 to 20 carbon atom(s); A2 is in particular a linear or branched alkylene radical including from 1 to 200 carbon atom(s); A3 is H or a linear or branched alkyl radical including from 1 to 15 carbon atom(s) and R1 and R1? are independently from each other H or a linear or branched alkyl radical comprising from 1 to 20 carbon atom(s). The compounds of formula (I) can be used in particular for the preparation of poly(hydroxyurethane)s and epoxy resins.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: March 27, 2018
    Assignees: UNIVERSITÉ DE BORDEAUX, INSTITUT POLYTECHNIQUE DE BORDEAUX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S), INSTITUT DES CORPS GRAS ETUDES ET RECHERCHES TECHNIQUES—ITERG
    Inventors: Henri Cramail, Etienne Grau, Carine Alfos, Lise Maisonneuve
  • Compositions, apparatus, systems, and methods for resolving electronic excited states
    Patent number: 9926289
    Abstract: The present disclosure relates, according to some embodiments, to molecules, including conjugated fused polycyclic molecules, that may receive excited state energy from other molecules (e.g., light-absorbing molecules) or directly from the irradiation sources. According to some embodiments, the disclosure relates to molecules, including conjugated fused polycyclic molecules, that may resolve (e.g., quench, dissipate) excited state energy, normally by way of releasing it as heat. (e.g., as heat). Conjugated fused polycyclic molecules of various structures are disclosed including Formula III: The disclosure further relates to methods of use and/or therapy using molecules of Formulas I, II, and/or III.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: March 27, 2018
    Inventors: Craig A. Bonda, Shengkui Hu, Qing Jean Zhang, Zhihui Zhang
  • Inhibitors of INV(16) leukemia
    Patent number: 9926290
    Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: March 27, 2018
    Assignee: University of Virginia Patent Foundation
    Inventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Mishra
  • Synthesis of thiohydantoins
    Patent number: 9926291
    Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: March 27, 2018
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Ouathek Ouerfelli, Anna Dilhas, Guangbin Yang, Hong Zhao
  • Pyridinyl derivatives, pharmaceutical compositions and uses thereof
    Patent number: 9926292
    Abstract: The invention relates to new pyridinyl derivatives of the formula wherein R1 and A are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: March 27, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Andreas Blum, Cédrickx Godbout, Joerg P. Hehn, Stefan Peters
  • Multivalent RAS binding compounds
    Patent number: 9926293
    Abstract: The present invention provides, inter alia, compounds having the structure: wherein R7, R8 and n are as disclosed herein, that selectively bind a RAS protein at two or more sites and methods for their synthesis. Compositions and kits containing the compounds, as well as methods of using the compounds and compositions for ameliorating or treating the effects of a disease associated with altered RAS signaling, such as a cancer, in a subject and methods for effecting cancer cell death are also provided herein. Methods of identifying a multivalent compound which binds selectively to a target protein also are provided herein.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: March 27, 2018
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Brent R. Stockwell, Matthew Welsch
  • Pesticidally active heterocyclic derivatives with sulphur containing substituents
    Patent number: 9926294
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: March 27, 2018
    Assignee: Syngenta Participations AG
    Inventors: Michel Muehlebach, Ruud Titulaer, Daniel Emery, Andrew Edmunds, Andre Stoller, Pierre Joseph Marcel Jung, Anke Buchholz, Peter Renold
  • Potent and selective inhibitors of hepatitis C virus
    Patent number: 9926295
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: March 27, 2018
    Assignees: Cocrystal Pharma, Inc., Emory University
    Inventors: Steven J. Coats, Richard Anthony Whitaker, Tamara Rosario McBrayer, Junxing Shi, Franck Amblard, Hongwang Zhang, Longhu Zhou, Raymond F. Schinazi
  • Process for the preparation of polymorphic forms of nilotinib hydrochloride
    Patent number: 9926296
    Abstract: A process for preparing Nilotinib hydrochloride Form R5 and Form R6 comprises: step a) providing a solution of Nilotinib free base in acetic acid and optionally an organic solvent, step b) adding hydrochloric acid taken in an organic solvent to the solution of step a), then separating Nilotinib hydrochloride Form R5 (step c), and finally drying at about 100° C. to 150° C. to obtain Nilotinib hydrochloride Form R6.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: March 27, 2018
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Arjun Kumar Tummala, Srinivas Rangineni
  • Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor agonists
    Patent number: 9926297
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: March 27, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Heterocyclic compounds and use thereof
    Patent number: 9926298
    Abstract: Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: March 27, 2018
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 9926299
    Abstract: The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolite, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and are further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provides the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: March 27, 2018
    Assignee: Centaurus BioPharma Co., Ltd.
    Inventors: Yongxin Han, Rong Yu, Zanping Wang, Zhi Liang, Quan Hu, Li Zhu, Yuandong Hu, Yinghui Sun, Na Zhao, Yong Peng, Xiaofeng Zhai, Hong Luo, Dengming Xiao
  • 5-acylsulfanyl-histidine compounds as precursors of the corresponding 5-sulfanylhistidines and their disulfides
    Patent number: 9926300
    Abstract: The invention relates to a compound of the 5-acylsulfanyl-histidine type and the derivatives thereof, of general formula (I), wherein R1 to R3=H, alkyl, especially CH3; R4=H, alkyl, especially CH3, alkyle(C=0), substituted alkyl (C?O), aryl (C?O); ?-alanyl (H2NCH2CH2 (C?O); ?-amino-acyl; R5=alkyl, especially methyl, phenyl. The invention also relates to the use of said compound for producing compounds of the 5-sulfanyl-histidine type and the derivatives thereof, in addition to corresponding disulfides; and to the various methods for the production thereof.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: March 27, 2018
    Assignee: TETRAHEDRON
    Inventors: Irene Erdelmeier, Sylvain Daunay
  • Bipyrazole derivatives as JAK inhibitors
    Patent number: 9926301
    Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: March 27, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, Song Mei
  • Heteroaryl substituted heterocyclyl sulfones
    Patent number: 9926302
    Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: January 12, 2017
    Date of Patent: March 27, 2018
    Assignee: GRÜNENTHAL GMBH
    Inventors: Stefan Schunk, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy Mackenzie